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 About 30 results found for searched term "MAPK-IN-2" (0.108 seconds)

Cat.No.  Name Target
M42115 MAPK-IN-2 EGFR/HER2
MAPK-IN-2 is a potent MAPK inhibitor with antineoplastic activity.
M1977 U0126-EtOH MEK
U0126
U0126-EtOH is a potent and highly selective non-competitive inhibitor of MAPK/ERK kinase with IC50 of 72 nM for MEK1 and 58 nM for MEK2.
M2090 MLN2480 Raf
BIIB-024; Tovorafenib
MLN2480 is an orally active, CNS-permeable, highly selective inhibitor of type II RAF kinase that inhibits both monomeric (class I mutant) and dimeric forms of RAF and does not cause aberrant activation of the MAPK pathway caused by type I RAF inhibitors. In addition, MLN2480 inhibits the growth of tumors harboring BRAF fusions or BRAF V600 mutations and can be used in studies related to gliomas.
M2198 Curcumin Histone Acetyltransferase
Indian Saffron; Turmeric yellow; Natural Yellow 3; Diferuloylmethane
Curcumin (Diferuloyl), a natural phenolic compound, is a p300/CREB binding protein specific inhibitor that inhibits histone/non-histone acetylation and histone acetyltransferase-dependent chromatin transcription. Curcumin inhibited NF-κ B and MAPKs, and had anti-inflammatory, antioxidant, anti-proliferation and anti-angiogenesis effects. Curcumin induces Nrf2 protein stabilization through Keap1 cysteine modification.
M3048 TAK-715 p38 MAPK
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
M5873 Pexmetinib (ARRY-614) p38 MAPK
ARRY-614
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
M6146 TA-02 p38 MAPK
TA 02; TA02
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
M6661 Deguelin Akt
(-)-Deguelin; (-)-cis-Deguelin
Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
M7582 SB 239063 p38 MAPK
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
M7792 EF-24 ERK
EF24
EF-24 is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively.
M9692 IAXO-102 TLR
Iaxo-102 is an antagonist of TLR4 and inhibits the TLR4 signaling pathway. Iaxo-102 inhibits phosphorylation of MAPK and P65 NF-KB and expression of TLR4 and TLR4-dependent inflammatory proteins. Iaxo-102 inhibits the development of experimental abdominal aortic aneurysms.
M14174 BMS-582949 hydrochloride p38 MAPK
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
M14176 MAPK13-IN-1 p38 MAPK
MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM.
M14177 p38-α MAPK-IN-1 p38 MAPK
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
M20012 CC-99677 Others
CC-99677 is an oral, covalent MAPK–activated protein kinase-2 (MK2) inhibitor being developed for autoimmune diseases.
M21938 BCI-215 Phosphatase
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
M28107 PF-3644022  MAPKAPK2/MAP3K/MAP4K
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
M28723 MW-150 p38 MAPK
MW01-18-150SRM
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
M28785 MW-150 dihydrochloride dihydrate p38 MAPK
MW01-18-150SRM dihydrochloride dihydrate
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
M28792 SD-169  p38 MAPK
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
M28863 PD-089828  FGFR
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
M29024 MW-150 hydrochloride p38 MAPK
MW01-18-150SRM hydrochloride
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
M29320 SHP2-IN-6  Phosphatase
JAB-3068
SHP2-IN-6 is a potent SHP2 inhibitor that interferes with the MAPK signaling pathway and inhibits the proliferation of SHP2-expressing tumor cells with an IC50 value of 25.8 nM.
M29321 SHP2-IN-6 hydrochloride  Phosphatase
JAB-3068 hydrochloride 
SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor that interferes with the MAPK signaling pathway and inhibits the proliferation of SHP2-expressing tumor cells with an IC50 value of 25.8 nM.
M29615 SR-318  p38 MAPK
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
M30587 Emprumapimod p38 MAPK
PF-07265803
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
M30703 12-Oxo phytodienoic acid NF-κB
12-OPDA
12-Oxo phytodienoic acid (12-OPDA, 12-oxo phytodienoic acid) is a plant lipid-derived compound with anti-inflammatory activity that inhibits neuroinflammation by inhibiting Nf-κB and p38 MAPK signaling in cells activated by lipopolysaccharide (LPS).12-Oxo phytodienoic acid can be used in the study of neurodegenerative diseases.
M30721 Ralimetinib p38 MAPK
LY2228820
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
M39013 Broussonin E ERK
Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis.
M45287 CK2/ERK8-IN-1 Casein Kinase
CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) (Ki 0.25 µM) and ERK8 (MAPK15, ERK7), both with IC50s of 0.50 µM. In addition, CK2/ERK8-IN-1 binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. 15.25 µM and 11.9 µM, respectively, and also has pro-apoptotic activity.



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